Volasertib

別名: BI 6727

目錄號(hào)：S2235 Purity: 99.78%

Volasertib是一種高度有效的Plk1抑制劑，無(wú)細(xì)胞試驗(yàn)中IC50為0.87 nM，比作用于Plk2和Plk3選擇性高6和65倍。Volasertib可在多種癌細(xì)胞中誘導(dǎo)細(xì)胞周期停滯和自噬。Phase 3。

Volasertib Chemical Structure

CAS: 755038-65-4

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	1654.53	現(xiàn)貨
5mg	974.11	現(xiàn)貨
25mg	3005.97	現(xiàn)貨
100mg	7125.3	現(xiàn)貨
1g	13677.3	現(xiàn)貨
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400-668-6834 info@selleck.cn

產(chǎn)品質(zhì)控

批次：純度： 99.78%

99.78

Volasertib相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	PLK1 PLK2 PLK3 PLK4	點(diǎn)擊展開(kāi)
相關(guān)產(chǎn)品	BI 2536 Rigosertib (ON-01910) GSK461364 Onvansertib (NMS-P937) SBE 13 HCl Ro3280 CFI-400945 HMN-214 MLN0905 Poloxin	點(diǎn)擊展開(kāi)
相關(guān)化合物庫(kù)	激酶抑制劑庫(kù) PI3K/Akt 抑制劑庫(kù) MAPK抑制劑庫(kù) DNA損傷/ DNA修復(fù)化合物庫(kù) 細(xì)胞周期化合物庫(kù)	點(diǎn)擊展開(kāi)

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類(lèi)型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
DU145	Growth Inhibition Assay	10/50/250 nM	24 h	IC50<10 nM	23884428
T98G	Growth Inhibition Assay	50-150 nM	72 h	inhibits cell proliferation	23887645
SF188	Growth Inhibition Assay	50-150 nM	72 h	inhibits cell proliferation	23887645
FaDu?	Growth Inhibition Assay	0-1000 nM	1-4 d	inhibits cell growth in both dose- and time-dependent manner	23891096
A431	Growth Inhibition Assay	0-30 nM	1-4 d	inhibits cell growth in both dose- and time-dependent manner	23891096
HCC1428/LTED	Growth Inhibition Assay	2.5-40 nM	5 d	inhibits cell growth in a dose-dependent manner	25480943
MCF7/LTED?	Growth Inhibition Assay	2.5-40 nM	5 d	inhibits cell growth in a dose-dependent manner	25480943
LNCaP	Growth Inhibition Assay	10/50/250 nM	24 h	IC50<10 nM	23884428
PC3	Growth Inhibition Assay	10/50/250 nM	24 h	IC50～600 nM	23884428
KMCH-1	Apoptosis Assay	200 nM	24 h	induces apoptosis	23703673
Mz-ChA-1	Apoptosis Assay	200 nM	24 h	induces apoptosis	23703673
HUCCT-1	Apoptosis Assay	200 nM	24 h	induces apoptosis	23703673
THP-1	Growth Inhibition Assay		72 h	IC50=56±39 nM	25576074
SKM-1	Growth Inhibition Assay		72 h	IC50=95±52 nM	25576074
OCI-AML3	Growth Inhibition Assay		72 h	IC50=90±51 nM	25576074
NOMO-1	Growth Inhibition Assay		72 h	IC50=145±7 nM	25576074
MV-4-11	Growth Inhibition Assay		72 h	IC50=16±6 nM	25576074
MOLM-13	Growth Inhibition Assay		72 h	IC50=57±44 nM	25576074
KG-1	Growth Inhibition Assay		72 h	IC50=150±67 nM	25576074
KASUMI-1	Growth Inhibition Assay		72 h	IC50=170±51 nM	25576074
RT4	Growth Inhibition Assay		48 h	IC50=111.27 nM	23792639
5637	Growth Inhibition Assay		48 h	IC50=1165.14 nM	23792639
T24	Growth Inhibition Assay		48 h	IC50=204.91 nM	23792639
SKBR3	Cytotoxicity assay		24 hrs	Cytotoxicity against human SKBR3 cells after 24 hrs by MTT assay	29288948
MDA-MB-231	Cytotoxicity assay		24 hrs	Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay	29288948
MDA-MB-468	Cytotoxicity assay		24 hrs	Cytotoxicity against human MDA-MB-468 cells after 24 hrs by MTT assay	29288948
BT474	Cytotoxicity assay		24 hrs	Cytotoxicity against human BT474 cells after 24 hrs by MTT assay	29288948
ZR-75-1	Cytotoxicity assay		24 hrs	Cytotoxicity against human ZR-75-1 cells after 24 hrs by MTT assay	29288948
HCT 116	Growth Inhibition Assay			EC50?= 23 nM	19383823
NCI-H460	Growth Inhibition Assay			EC50?= 21 nM	19383823
BRO	Growth Inhibition Assay			EC50?= 11 nM	19383823
GRANTA-519	Growth Inhibition Assay			EC50?= 15 nM	19383823
HL-60	Growth Inhibition Assay			EC50?= 32 nM	19383823
THP-1	Growth Inhibition Assay			EC50 = 36 nM	19383823
Raji	Growth Inhibition Assay			EC50 = 37 nM	19383823
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

特性

BI6727具有高的體積分布，良好的組織穿透力和長(zhǎng)的半衰期。

靶點(diǎn)

PLK1 ^[1]
(Cell-free assay)

0.87 nM

體外研究(In Vitro)
體外研究活性	如同BI2536，BI6727是屬于dihydropteridinone類(lèi)化合物的ATP競(jìng)爭(zhēng)性激酶抑制劑。除了Plk1，BI6727也有效地抑制兩個(gè)密切相關(guān)的激酶Plk2和Plk3，IC50分別為為5 nM和56 nM。 BI6727在濃度高達(dá)10 μM時(shí)對(duì)五十多種激酶均沒(méi)有抑制活性。BI6727抑制從各種癌組織來(lái)源的多種細(xì)胞系的增殖，包括HCT116, NCI-H460, BRO, GRANTA-519, HL-60, THP-1 和 Raji 細(xì)胞，EC50 分別為23 nM, 21 nM, 11 nM, 15 nM, 32 nM, 36 nM 和 37 nM。在NCI-H460細(xì)胞中，BI6727 (100 nM)誘導(dǎo)有絲分裂細(xì)胞聚集，這些細(xì)胞中有單極紡錘體和組蛋白H3的磷酸絲氨酸10陽(yáng)性染色，這表明細(xì)胞處于M期，隨后誘導(dǎo)細(xì)胞凋亡。^[1] BI6727低納摩爾濃度表現(xiàn)對(duì)神經(jīng)母細(xì)胞瘤（NB）腫瘤起始細(xì)胞（NB TIC）的抑制活性，EC 50為21 nM，而只有微摩爾濃度的BI6727對(duì)正常小兒神經(jīng)干細(xì)胞有毒性作用。^[2] 類(lèi)似于BI2536，BI6727誘導(dǎo)Daoy和ONS-76髓母細(xì)胞瘤細(xì)胞的生長(zhǎng)停滯。^[3]
激酶實(shí)驗(yàn)	體外激酶抑制試驗(yàn)
激酶實(shí)驗(yàn)	重組人類(lèi)Plk1的（殘基1-603）是用桿狀病毒表達(dá)系統(tǒng)表達(dá)的帶有NH₂末端和GST-標(biāo)記的融合采用的蛋白質(zhì)。酶的活性測(cè)定法測(cè)定Plk1是在梯度稀釋的BI6727中進(jìn)行，以20 ng重組激酶以及10 μg牛乳酪蛋白為底物。激酶反應(yīng)在60微升的終體積在30℃下進(jìn)行45分鐘[15 mM MgCl₂, 25 mM MOPS (pH 7.0), 1 mM DTT, 1% DMSO, 7.5 μM ATP, 0.3 μCi γ-³²P-ATP]。反應(yīng)通過(guò)加入125μL冰冷的5％三氯乙酸終止。轉(zhuǎn)移沉淀到多屏幕混合酯纖維素過(guò)濾板后，洗滌板用1％三氯乙酸洗滌并測(cè)量輻射量。劑量-反應(yīng)曲線用于計(jì)算IC 50值。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	HCT116，NCI-H460，BRO，GRANTA-519，HL-60，THP-1，和Raji細(xì)胞
	濃度	溶解在DMSO中至終濃度約1 μM
	孵育時(shí)間	24, 48和72小時(shí)
	方法	細(xì)胞增殖測(cè)定是將細(xì)胞孵育在不同濃度的BI6727中24，48和72小時(shí)，而后在熒光分光光度計(jì)上通過(guò)測(cè)量的Alamar藍(lán)染料的轉(zhuǎn)換測(cè)定。有效濃度在哪些細(xì)胞生長(zhǎng)是由50％（EC 50）抑制從劑量 - 反應(yīng)曲線擬合推斷的。為了確定DNA含量，細(xì)胞懸浮液被固定在80％乙醇中，用含0.25％Triton X-100的PBS處理5分鐘，并用含0.1％RNA酶和10 μg/mL的碘化丙錠的PBS室溫孵育20分鐘。細(xì)胞周期的測(cè)定是用流式細(xì)胞儀分析的。
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)圖片	PMID
	Western blot	Fibronectin / β-integrin / p-vimentin / Vimentin / p-HH3 p-c-Met / c-Met / p-FAK / FAK / p-Src / Src PARP / c-myc p-AKT / AKT / p-MAPK / MAPK p-PLK1 / PLK1		31040125
	Immunofluorescence	PLK1 / Wee1		29108241
	Growth inhibition assay	Cell viability		29383095

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	BI6727顯著抑制多種人類(lèi)腫瘤異種移植物的生長(zhǎng)，包括HCT116, NCI-H460, 和紫杉類(lèi)耐藥CXB1結(jié)腸癌，伴隨著增加的有絲分裂指數(shù)以及細(xì)胞凋亡的增加。^[1] 體內(nèi)研究表明，BI6727表現(xiàn)出比BI2536更好的毒性和藥動(dòng)學(xué)特征。^[3]
動(dòng)物實(shí)驗(yàn)	Animal Models	雌性BomTac：NMRI-Foxn1^{NU小鼠腹腔移植HCT116，NCI-H460，或CXB1細(xì)胞。}
	Dosages	約25 mg/kg/day
	Administration	靜脈注射，或通過(guò)灌胃針

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT02722135	Withdrawn	Leukemia Myeloid Acute	Boehringer Ingelheim	November 2016	Phase 1
NCT02721875	Terminated	Myelodysplastic Syndromes	Boehringer Ingelheim	April 28 2016	Phase 1
NCT02201329	Completed	Myelodysplastic Syndromes\|Leukemia Myelomonocytic Chronic	Boehringer Ingelheim	August 2014	Phase 1
NCT01971476	Completed	Leukemia\|Neoplasms	Boehringer Ingelheim	October 22 2013	Phase 1
NCT01772563	Completed	Neoplasms	Boehringer Ingelheim	February 4 2013	Phase 1
NCT01662505	Completed	Leukemia Myeloid Acute	Boehringer Ingelheim	August 2012	Phase 1

參考文獻(xiàn)
[1] Rudolph D, et al. Clin Cancer Res, 2009, 15(9), 3094-3102. [2] Grinshtein N, et al. Cancer Res, 2011, 71(4), 1385-1395. [3] Harris PS, et al. BMC Cancer, 2012, 12, 80.

參考文獻(xiàn)

[1] Rudolph D, et al. Clin Cancer Res, 2009, 15(9), 3094-3102.
[2] Grinshtein N, et al. Cancer Res, 2011, 71(4), 1385-1395.
[3] Harris PS, et al. BMC Cancer, 2012, 12, 80.

化學(xué)信息&溶解度

分子量	618.81	分子式	C₃₄H₅₀N₈O₃
CAS號(hào)	755038-65-4	SDF	Download Volasertib SDF
Smiles	CCC1C(=O)N(C2=CN=C(N=C2N1C(C)C)NC3=C(C=C(C=C3)C(=O)NC4CCC(CC4)N5CCN(CC5)CC6CC6)OC)C
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 35 mg/mL ( (56.56 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 30 mg/mL ( (48.48 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 20 mg/mL ( (32.32 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 20 mg/mL ( (32.32 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

技術(shù)支持

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操作手冊(cè)

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* 必填項(xiàng)

常見(jiàn)問(wèn)題及建議解決方法

問(wèn)題 1:
I wonder how to reconstitute the inhibitor for in vivo studies?

回答：
Volasertib can be dissolved in 4% DMSO+Corn oil at 2mg/ml for i.p. injection in mice. For oral administration, it can be formulated in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl, or suspended in 0.5% Natrosol 250 hydroxyethyl-cellulose as indicated in the publications. We also suggest the vehicle 30% PEG400/0.5% Tween80/5% propylene glycol for a suspension which we tested in house.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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Volasertib

產(chǎn)品質(zhì)控

Volasertib相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實(shí)驗(yàn)計(jì)算

技術(shù)支持

常見(jiàn)問(wèn)題及建議解決方法